| DA801002 (in Galluppi 2021) |
Population pharmacokinetic analysis of ulotaront in
subjects with schizophrenia |
DA801002 |
Sunovion/Sumitomo |
SB-RCT single ascending dose (phase I) |
Men >18 years |
Ulotaront (25mg to 50mg); Placebo |
16 |
Pharmacokinetics |
NA |
NA |
2021 |
completed |
None |
| Fowler (2015) |
A UGT2B10 Splicing Polymorphism Common in African
Populations May Greatly Increase Drug Exposure |
NA |
Hoffmann-La Roche |
DB-RCT; single ascending dose (phase I) |
Men 18-45 years |
RO5263397 (1mg to 125mg); Placebo |
49 |
Tolerability, pharmacokinetics |
NA |
NA |
2015 |
completed |
None |
| Hopkins (2021) |
Effect of TAAR1/5-HT1A agonist SEP-363856 on REM sleep
in humans |
SEP361-103 |
Sunovion/Sumitomo |
DB-RCT two-period crossover; single dose (phase I) |
Men 18-35 years |
Cohort 1: Ulotaront 10mg; Placebo; Cohort 2: Ulotaront
50mg; Placebo |
24 |
Sleep parameters, pharmacokinetics |
NA |
NA |
2021 |
completed |
Dropouts, side-effects |
| Isaacson (2023) |
Ulotaront, a Trace Amine-Associated Receptor
1/Serotonin 5-HT1A Agonist, in Patients With Parkinson Disease
Psychosis: A Pilot Study. |
SEP361-203, NCT02969369 |
Sunovion/Sumitomo |
DB-RCT; 6 weeks (with open label extension) (phase
2) |
Men/women ≥55 years with Parkinson’s disease psychosis
(acute) |
Ulotaront 20-75mg/d; Placebo |
39 |
Efficacy (acute), safety |
21.11.16 |
05.07.23 |
2023 |
completed |
Efficacy, dropouts, side-effects |
| JapicCTI-194581 (2019) |
A Phase I Single-Ascending Dose and Multiple-Ascending
Dose Study of RO6889450 in Healthy Japanese Male |
JapicCTI-194581 |
Hoffmann-La Roche |
DB-RCT; single and multiple ascending dose (phase
I) |
Men 20-45 years |
Ralmitaront; Placebo |
64 |
Tolerability, pharmacokinetics |
27.01.19 |
23.10.19 |
2019 |
completed |
None |
| Koblan (2016) |
A phase 1 open label safety and tolerability study of
SEP-363856, a novel NON-D2 mechanism of action molecule, in patients
with schizophrenia |
SEP361-106, NCT01994473 |
Sunovion/Sumitomo |
SB-RCT; multiple ascending dose for 1 week (including
open label extension) (phase 1) |
Men/women 18-55 years with schizophrenia (stable,
DSM-IV-TR) |
Ulotaront (10mg/d to 100mg/d); Placebo |
48 |
Tolerability, pharmacokinetics |
41334 |
41974 |
2014 |
completed |
None |
| Koblan (2020) |
A Non–D2-Receptor-Binding Drug for the Treatment of
Schizophrenia |
SEP361-201, NCT02969382, EUCTR2016-001555-41 |
Sunovion/Sumitomo |
DB-RCT; 4 weeks (with open label extension) (phase
2) |
Men/women 18-40 years with schizophrenia (acute,
DSM-5) |
Ulotaront (50-75mg/d); Placebo |
245 |
Efficacy (acute), tolerability |
05.12.16 |
31.07.18 |
2018 |
completed |
Efficacy, dropouts, side-effects |
| NCT01940159 (2013) |
A Study Assessing the Safety, Tolerability, and
Pharmacokinetics of SEP-363856 in Male and Female Subjects With
Schizophrenia |
SEP361-105, NCT01940159 |
Sunovion/Sumitomo |
SB-RCT; single ascending dose (phase 1) |
Men/women 18-50 years with schizophrenia (stable,
DSM-IV-TR) |
Ulotaront (50mg to 150mg); Placebo |
48 |
Tolerability, pharmacokinetics |
41334 |
41730 |
2014 |
completed |
None |
| NCT02699372 (2016) |
The Safety, Tolerability, Pharmacokinetics and
Pharmacodynamics Study of RO6889450 in Healthy Volunteers |
BP30134, NCT02699372 |
Hoffmann-La Roche |
DB-RCT; single and multiple ascending dose up to 2
weeks (phase I) |
Men/women 18-45 years |
Ralmitaront (5 mg to 450mg); Placebo |
164 |
Tolerability, pharmacokinetics |
21.03.16 |
14.04.17 |
2017 |
completed |
None |
| NCT03669640 (2018) |
A Study to Assess the Effects of RO6889450
(Ralmitaront) in Participants With Schizophrenia or Schizoaffective
Disorder and Negative Symptoms |
BP40283, NCT03669640, EUCTR2020-004752-16,
JPRN-jRCT2031200287 |
Hoffmann-La Roche |
DB-RCT; 12 weeks (phase II) |
Men/women 18-55 years with schizophrenia or
schizoaffective (predominant negative symptoms, DSM-5) |
Part A: Ralmitaront; placebo (monotherapy); Part B:
Ralmitaront low or high dose; placebo (add-on to current
antipsychotics) |
128 |
Efficacy (negative symptoms), tolerability |
04.12.18 |
08.05.23 |
2023 |
completed |
None |
| NCT04072354 (2019) |
A Clinical Trial to Study the Efficacy and Safety of an
Investigational Drug in Acutely Psychotic People With Schizophrenia |
SEP361-301, NCT04072354, EUCTR2019-000470-36 |
Sunovion/Sumitomo |
DB-RCT; 6 weeks (phase 3) |
Men/women 13-17 and 18-65 years with schizophrenia
(acute, DSM-5) |
Ulotaront 50mg/d; Ulotaront 75mg/d; Placebo |
463 |
Efficacy (acute), tolerability |
11.09.19 |
08.06.23 |
2023 |
completed |
Efficacy, dropouts |
| NCT04092686 (2019) |
A Clinical Trial That Will Study the Efficacy and
Safety of an Investigational Drug in Acutely Psychotic People With
Schizophrenia |
SEP361-302, NCT04092686, EUCTR2019-000697-37 |
Sunovion/Sumitomo |
DB-RCT; 6 weeks (phase 3) |
Men/women 18-65 years with schizophrenia (acute,
DSM-5) |
Ulotaront 75mg/d; Ulotaront 100mg/d; Placebo |
462 |
Efficacy (acute), tolerability |
30.09.19 |
08.09.23 |
2023 |
completed |
Efficacy, dropouts |
| NCT04115319 (2019) |
A Study of the Long-term Safety and Tolerability of an
Investigational Drug in People With Schizophrenia. |
SEP361-304, NCT04115319 , EUCTR2019-002259-40 |
Sunovion/Sumitomo |
DB-RCT; 52 weeks (phase 3) |
Men/women 18-65 years with schizophrenia (stable,
DSM-5) |
Ulotaront 50-100mg/d; Quetiapine XR 400-800mg/d |
475 |
Efficacy (maintenance), tolerability |
15.11.19 |
30.12.22 |
2022 |
completed |
None |
| NCT04325737 (2020) |
Study Assessing the Safety, Tolerability, and
Pharmacokinetics of SEP-363856 in Japanese Male and Female Subjects With
Schizophrenia |
DA801102, NCT04325737, jRCT2080225100 |
Sunovion/Sumitomo |
DB-RCT; 2 weeks (phase 1) |
Men/women 18-65 years with schizophrenia (stable,
DSM-5) |
Cohort 1: Ulotaront (50mg/d to 100mg/d); Placebo;
Cohort 2: Ulotaront (25mg/d to 100mg/d); Placebo |
13 |
Tolerability, pharmacokinetics |
31.03.20 |
07.08.20 |
2020 |
completed |
None |
| NCT04512066 (2020) |
A Trial of the Efficacy and the Safety of RO6889450
(Ralmitaront) vs Placebo in Patients With an Acute Exacerbation of
Schizophrenia or Schizoaffective Disorder |
BP41743, NCT04512066, JPRN-jRCT2031200288 |
Hoffmann-La Roche |
DB-RCT; 8 weeks (up to 48 weeks extension) (phase
II) |
Men/women 18-45 years with schizophrenia or
schizoaffective disorder (acute, DSM-5) |
Ralmitaront 45mg/d; Ralmitaront 150mg/d; Risperidone
4mg/d; Placebo |
287 |
Efficacy (acute), tolerability |
08.09.20 |
21.06.22 |
2022 |
completed |
Efficacy, dropouts, side-effects |
| NCT04825860 (2021) |
A Clinical Trial to Evaluate the Efficacy and Safety of
SEP-363856 in Acutely Psychotic People With Schizophrenia, Followed by
an Open-label Extension Phase |
DA801201, NCT04825860, jRCT2071210003 |
Sunovion/Sumitomo |
DB-RCT; 6 weeks (and open label extension) (phase
2/3) |
Men/women 18-65 years with schizophrenia (acute,
DSM-5) |
Ulotaront 50mg/d; Ulotaront 75mg/d; Placebo |
480 |
Efficacy (acute), tolerability |
29.03.21 |
30.06.25 |
NA |
ongoing |
None |
| NCT05402111 (2022) |
A Clinical Study That Will Assess How Food Moves
Through the Stomach and Effects Blood Glucose Levels in Subjects With
Schizophrenia Taking SEP-363856 or and Prior Antipsychotic (PA)
Standard |
SEP361-124, NCT05402111 (2022) |
Sunovion/Sumitomo |
Open RCT two-period crossover; single dose (phase
1) |
Men/women 18-65 years with schizophrenia (stable,
DSM-5) |
Ulotaront (25mg to 50mg); Prior antipsychotics
(risperidone, olanzapine, quetiapine, aripiprazole) |
36 |
Pharmacokinetics, metabolic parameters |
13.06.22 |
13.07.23 |
NA |
ongoing |
None |
| NCT05542264 (2022) |
A Clinical Study That Will Assess the Effect of
SEP-363856 or Prior Antipsychotic (PA) Standard of Care on Body-weight
Associated Parameters in Subjects With Schizophrenia |
SEP361-122, NCT05542264 |
Sunovion/Sumitomo |
DB-RCT; 2 weeks (phase 1) |
Men/women 18-65 years with schizophrenia (stable,
DSM-5) |
Ulotaront; Prior antipsychotics (risperidone,
olanzapine, quetiapine, aripiprazole) |
60 |
Metabolic parameters |
15.11.22 |
23.10.23 |
NA |
ongoing |
None |
| NCT05593029 (2022) |
A Trial of the Safety and Efficacy of SEP-363856 in the
Treatment of Adults With Major Depressive Disorder |
382-201-00001, NCT05593029 |
Sunovion/Sumitomo |
DB-RCT; 14 weeks (phase 2/3) |
Men/women 18-65 years with MDD (acute, DSM-5) |
Ulotaront; Placebo (add-on to antidepressants) |
900 |
Efficacy (MDD), tolerability |
09.11.22 |
45778 |
NA |
ongoing |
None |
| NCT05729373 (2023) |
A Clinical Study That Will Meaure How Well SEP-363856
Works and How Safe it is in Adults With Generalized Anixety
Disorder |
SEP361-226, NCT05729373, EUCTR2022-502077-42-00 |
Sunovion/Sumitomo |
DB-RCT; 8 weeks (phase 2/3) |
Men/women 18-65 years with GAD (acute, DSM-5) |
Ulotaront (50-75mg/d); Placebo |
464 |
Efficacy (GAD), tolerability |
08.03.23 |
08.02.25 |
NA |
ongoing |
None |
| NCT05848700 (2023) |
A Clinical Study to Learn if SEP-363856 Has Physical
Dependence in Adults With Schizophrenia |
SEP361-121, NCT05848700 |
Sunovion/Sumitomo |
DB-RCT; 10 weeks (phase 1) |
Men/women 18-65 years with schizophrenia (stable,
DSM-5) |
Ulotaront continuation; Ulotaront discontinuation
(switch to placebo) |
60 |
Physical dependence, pharmacokinetics |
21.06.23 |
23.02.24 |
NA |
ongoing |
None |
| Perini (2023) |
Effects of ulotaront on brain circuits of reward,
working memory, and emotion processing in healthy volunteers with high
or low schizotypy |
SEP361-104, NCT01972711 |
Sunovion/Sumitomo |
DB-RCT; single dose (phase 1) |
Men/women 18-45 years (high or low levels of
schizotypy) |
Ulotaront 50mg; Amisulpride 400mg; Placebo |
105 |
fMRI |
41699 |
42186 |
2015 |
completed |
Dropouts, side-effects |
| SEP361-101 (in Galluppi 2021 and Chen 2022) |
A sensitive LC-MS/MS method for simultaneous
quantification of ulotaront and its N-desmethyl metabolite in human
plasma and application to a clinical study |
SEP361-101 |
Sunovion/Sumitomo |
SB-RCT; single ascending dose (phase I) |
Men >18 years |
Ulotaront (5mg to 125mg); Placebo |
52 |
Pharmacokinetics |
NA |
NA |
2021 |
completed |
None |
| Szabo (2023) |
A multicenter, double-blind, placebo-controlled,
randomized, Phase 1b crossover trial comparing two doses of ulotaront
with placebo in the treatment of narcolepsy-cataplexy. |
SEP361-108 , NCT05015673 |
Sunovion/Sumitomo |
DB-RCT three-period crossover; 2 weeks (phase 1) |
Men/women 18-55 years with narcolepsy/cataplexy |
Ulotaront 25mg; Ulotaront 50mg; Placebo |
18 |
Sleep parameters, pharmacokinetics, tolerability |
05.06.14 |
26.05.15 |
2015 |
completed |
Dropouts, side-effects |
| Tsukada (2023) |
A randomized, single-dose, crossover study of the
effects of ulotaront on electrocardiogram intervals in subjects with
schizophrenia. |
SEP361-114, NCT04369391 |
Sunovion/Sumitomo |
DB-RCT three-period crossover; single dose (phase
1) |
Men/women 18-65 years with schizophrenia (stable,
DSM-5) |
Ulotaront 150mg; Placebo; Moxifloxacin 400mg
(ineligible for the review) |
68 |
QTc interval, tolerability, pharmacokinetics |
18.06.20 |
10.11.20 |
2020 |
completed |
Dropouts, side-effects |